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Compound Detail

CHEMBL1780224

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CCN(CC)c1ccc2nc3c4ccccc4/c(=N\c4ccncc4)cc-3oc2c1

Basic Information

ChEMBL ID CHEMBL1780224
Phase Preclinical
Structure Type MOL
InChI Key HBSWMATYASLRBW-QYQHSDTDSA-N
5
Targets
7
Activities
1
Assay Types
2
PK Parameters
14
Publications
0
Known Names

Molecular Properties

394.5
MW (Da)
5.56
ALogP
5
HBA
0
HBD
54.5
PSA (Ų)
0.30
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H22N4O
MW 394.48
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.01

Activity Summary

IC50 7 meas. best 8.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 8.19 8.09 6.5 3
Leishmania donovani
CHEMBL367
IC50 5.19 5.19 6500.0 1
Trypanosoma cruzi
CHEMBL368
IC50 4.95 4.95 11300.0 1
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 4.44 4.44 36000.0 1
L6
CHEMBL614793
IC50 4.25 4.25 55700.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 30.0 % Rattus norvegicus
T1/2 5.5 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24900219 10.1021/ml100120a Plasmodium berghei 13
24900219 10.1021/ml100120a Unchecked 4
24900219 10.1021/ml100120a ADMET 4
24900219 10.1021/ml100120a Mus musculus 3
24900219 10.1021/ml100120a Rattus norvegicus 2
24856305 10.1016/j.bmc.2014.04.066 Plasmodium falciparum 2
24900219 10.1021/ml100120a Plasmodium falciparum 1
24900219 10.1021/ml100120a L6 1
24900219 10.1021/ml100120a Adenosine receptor A3 1
24900219 10.1021/ml100120a D(3) dopamine receptor 1
24900219 10.1021/ml100120a Trypanosoma brucei rhodesiense 1
24900219 10.1021/ml100120a Trypanosoma cruzi 1
24900219 10.1021/ml100120a Leishmania donovani 1
24900219 10.1021/ml100120a Blood 1

Data from ChEMBL 36 via Core Engine